Estrace (Estradiol)

Progynova, Climaval

Prescription Required
Brand
Dose Size & Price Qty
0.5mg
1mg
2mg
Generic
Dose Size & Price Qty
0.5mg
1mg
2mg
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Fact Table

Fact Table
Formula C18H24O2
License FDA approved (1975)
Bioavailability ~5% orally (low due to extensive first-pass metabolism)
Legal status Prescription only (Rx)
Chemical Name estra-1,3,5(10)-triene-3,17ß-diol
Elimination half-life Oral: ~13–20 hours
Dosage (Strength) 0.5 mg, 1 mg, and 2 mg oral tablets
Pregnancy Contraindicated; should not be used during pregnancy
Brands Estrace; generic estradiol tablets available
Protein binding >95% (primarily to SHBG and albumin)
PubChem CID 5757
MedlinePlus a682922
ChEBI 23965
ATC code G03CA03
DrugBank DB00783
KEGG D00105
Routes of administration By mouth (oral tablets)

Estrace (estradiol) is an estrogen replacement therapy used to treat menopausal symptoms in women. The medication contains micronized estradiol, the same form of estrogen that women's ovaries naturally produce before menopause. By replacing the estrogen the body no longer makes, Estrace helps relieve common menopause symptoms like hot flashes and vaginal dryness. It's available as tablets in 0.5, 1, or 2 mg strengths, as well as a vaginal cream.

Directions

Estrace tablets should be taken by mouth at the same time each day, with or without food. For treating moderate to severe symptoms caused by menopause, the usual starting dosage ranges from 1 to 2 mg daily. Some people may require doses as low as 0.5 mg or as high as 6 mg per day.

A healthcare provider will determine the appropriate dose based on symptoms and treatment response. When used for conditions like female hypogonadism or primary ovarian failure, dosing may vary and involve cyclic administration, which means taking the medication for three weeks followed by one week off.

Those who use Estrace as part of a fertility treatment protocol should follow their clinic's specific instructions. It's important to use the lowest effective dose for the shortest duration needed to manage symptoms. Do not stop the medication abruptly without consulting a healthcare provider.

Ingredients

The active ingredient in Estrace is estradiol.

Cautions

Before using this medication, you may want to consult a healthcare provider about the following:

  • Any existing health conditions
  • Any allergies
  • A list of all medications currently being taken
  • Estrogen therapy like Estrace may increase the risk of serious cardiovascular events, including deep vein clots (DVT) and pulmonary embolism (PE). Stop Estrace and get emergency help if you have chest pain, sudden shortness of breath, coughing blood, one-sided leg swelling, sudden weakness, or trouble speaking.
  • Stop before certain surgeries or long periods of bed rest. If possible, estrogens are usually stopped 4 to 6 weeks before surgery that increases clot risk.
  • Using estrogen alone in someone who still has a uterus may increase the risk of endometrial (uterine) cancer, especially with longer use or higher doses. Report any unusual vaginal bleeding right away.
  • Breast cancer risk may increase with long-term use. Estrogen (especially when combined with a progestin) has been linked to a higher risk of breast cancer in some studies. Keep up with routine breast exams and mammograms based on your age and risk factors.
  • In studies of women age 65 and older, estrogen plus progestin was linked to a higher risk of probable dementia; it’s not clear if this applies to estrogen-only therapy.
  • Gallbladder problems can happen. Estrogens have been linked to a higher risk of gallbladder disease that may require surgery.
  • Vision changes are an emergency. Rarely, blood clots in the eye have been reported; stop Estrace and get checked urgently for sudden vision loss, new double vision, bulging of the eye, or a sudden severe migraine-like headache.
  • Certain health conditions need extra caution. Estrace can worsen issues like high triglycerides (which can trigger pancreatitis), liver problems, fluid retention, migraines, asthma, diabetes, epilepsy, or lupus.
  • Estrogen can change thyroid hormone binding, so some people on thyroid replacement may need a dose adjustment and monitoring.
  • Estrace should not be used during pregnancy, and it may reduce breast milk supply and pass into milk. Discuss potential risks and benefits if you’re nursing.
  • Estrace 2 mg contains FD and C Yellow No. 5 (tartrazine), which can rarely trigger allergic-type reactions (including asthma), especially in people sensitive to aspirin.

Contraindications

Avoid taking or using this medication if any of the following apply:

  • Unexplained abnormal vaginal or genital bleeding
  • Known, suspected, or prior breast cancer (except in carefully selected patients treated for metastatic disease)
  • Known or suspected cancers that depend on estrogen for growth
  • Current or past deep vein thrombosis or pulmonary embolism
  • Current or recent arterial blood clots, including stroke or heart attack
  • Liver disease or impaired liver function
  • Known allergy or sensitivity to estradiol or any component of the product, including FD and C Yellow No. 5 (tartrazine), which may cause allergic reactions—especially in people with aspirin sensitivity
  • Known or suspected pregnancy (this medication is not indicated during pregnancy)

Side Effects

Common side effects of Estrace include:

  • Headache
  • Breast tenderness or pain
  • Irregular vaginal bleeding or spotting
  • Nausea or stomach bloating

These side effects are usually mild and may occur as your body adjusts to estrogen therapy. Some people may also notice abdominal cramps, vomiting, hair thinning, or fluid retention. Vaginal yeast infections and dark patches of skin on the face can also occur in some individuals.

More serious side effects are less common but possible. Estrogen medicines like Estrace may increase the risk of blood clots, stroke, heart attack, breast cancer, uterine cancer, and gallbladder disease. Warning signs include unusual vaginal bleeding, breast lumps, severe headaches, chest pain, shortness of breath, leg pain, vision changes, or dizziness.

Frequently Asked Questions about Estrace (Estradiol)


What is Estrace used for?

Estrace is a brand name for estradiol, a form of estrogen hormone therapy. Depending on the product form, it is used to treat certain menopausal symptoms such as hot flashes, vaginal dryness, burning, and irritation, and in some cases other estrogen-deficiency states.


Is Estrace available in more than one form?

Yes. Estrace has been available as oral tablets and as a vaginal cream. The form matters because oral estradiol is used more for systemic symptoms like hot flashes, while vaginal estradiol is commonly used for local menopausal symptoms affecting the vagina and vulva.


How is Estrace usually used?

Oral Estrace is typically taken by mouth once daily as prescribed. Estrace vaginal cream is applied into the vagina on the schedule directed by a clinician, which may be daily at first and then reduced to a maintenance schedule. It should be used exactly as directed.


What are the most common side effects of Estrace?

Common side effects can include headache, breast tenderness, nausea, bloating, abdominal discomfort, vaginal spotting or bleeding, and fluid retention. Vaginal cream may also cause local irritation or discharge. Side effects vary depending on dose and product form.


Are there serious warnings with Estrace?

Yes. Estrogen therapy can increase the risk of blood clots, stroke, and certain cancers in some patients. In women with a uterus, using estrogen without a progestin can increase the risk of endometrial cancer. Unusual vaginal bleeding should always be evaluated.


Who should not usually use Estrace?

Estrace is generally avoided in people with undiagnosed abnormal genital bleeding, known or suspected estrogen-dependent cancers, active or past blood clots in certain situations, liver disease, or known allergy to estradiol products. It is also generally not used during pregnancy.


Does Estrace need to be used with another hormone?

Sometimes. Women who still have a uterus may need a progestin along with systemic estrogen therapy to reduce the risk of endometrial hyperplasia and endometrial cancer. This does not apply in the same way to every product or every patient, so treatment is individualized.


Can Estrace interact with other medicines?

Yes. Some medicines can change estradiol levels or increase side effects, including certain seizure medicines, antibiotics like rifampin, some antifungals, and other hormone-related therapies. All prescription medicines, over-the-counter products, and supplements should be reviewed before starting it.


What should someone do if they miss a dose?

A missed dose is usually taken when remembered unless it is almost time for the next dose. If it is close to the next dose, the missed dose is skipped and the regular schedule is resumed. Two doses should not be used at the same time unless specifically instructed.


What is the general approach to using Estrace safely?

Estrace is usually prescribed at the lowest effective dose for the shortest appropriate duration based on the treatment goal. Regular follow-up is important so symptoms, side effects, breast health, and any abnormal bleeding can be reviewed during treatment.

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